The present invention relates to novel, pharmacologically active compounds, methods for their preparation and their therapeutic use. The invention also relates to pharmaceutical compositions containing the compounds. More particularly, the novel compounds of the invention are intended for the treatment of chronic obstructive airway disease (COAD) and cardiovascular diseases.
Theophylline and various salts thereof are used in the treatment of chronic obstructive airway disease (COAD) and cardiac disease. Major therapeutic effects of theophylline are to relax bronchial smooth muscle and stimulate heart muscle. The major drawback with theophylline therapy is that the drug frequently produces toxic side effects; most common are nausea and gastric distress, most serious are convulsions, which may lead to death.
The object of the present invention is to provide xanthine derivatives which are more potent than theophylline. Another object of the present invention is to provide xanthine derivatives which have a bronchodilatory and cardiovascular potency, but which do not produce drowsiness.
Certain xanthine derivatives, in particular the 1,3,8-trialkylxanthines having a 1-methyl group combined with a group having 4-7 carbon atoms in the 3-position, are used in the treatment of bronchial asthma and other bronchospastic and allergic diseases. The major drawback with 1,3,8-trialkylxanthine therapy is that such drugs frequently produce behavioral side effects, such as drowsiness. Thus, a patient so treated must cope with an impaired level of alertness. In these instances, operation of heavy machinery or driving a car would be contraindicated.